| MonastrolEg5 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 99.25%
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| Cas No. | 329689-23-8 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | ethyl 6-(3-hydroxyphenyl)-2-mercapto-4-methyl-1,6-dihydropyrimidine-5-carboxylate | ||
| Canonical SMILES | CCOC(C(C1C2=CC(O)=CC=C2)=C(N=C(S)N1)C)=O | ||
| Formula | C14H16N2O3S | M.Wt | 292.35 |
| Solubility | ≥29.2mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 14 μM
Monastrol is a cell-permeable small molecule inhibitor of the mitotic kinesin, Eg5. Like other kinesins, Eg5 can drive the movement of microtubules in vitro.
In vitro: Previous study found that monastrol did not inhibit progression through S and G2 phases of the cell cycle or centrosome duplication. The mitotic arrest due to monastrol was also reversible rapidly. Chromosomes in monastrol-treated cells frequently had both sister kinetochores attached to microtubules extending to the center of the monoaster. Monastrol also inhibited bipolar spindle formation in Xenopus egg extracts, however, monastrol did not prevent the targeting of Eg5 to the monoastral spindles that form [1].
In vivo: Previous study investigated the rat PK and TK of LaSOM 65, a monastrol derivative. Results showed that LaSOM 65 had good bioavailability and linear PK after oral doses. LaSOM 65 distributed consistently in lung and fatty tissues. Other investigated tissues presented smaller penetration ratios. Adverse symptoms were observed only after iv administration, and regressed 3 h after dosing. No statistical differences were found for serum analysis, body weight and relative organ weight, indicating no acute toxicological effects. [2].
Clinical trial: Up to now, LaSOM 65 is still in the preclinical development stage.
References:[1] Kapoor TM,Mayer TU,Coughlin ML,Mitchison TJ. Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5. J Cell Biol.2000 Sep 4;150(5):975-88.[2] Torres BG,Ucha Fde T,Pigatto MC,Azeredo FJ,Haas SE,Dallegrave E,Canto RF,Eifler-Lima VL,Dalla Costa T. Pre-clinical pharmacokinetics and acute toxicological evaluation of a monastrol derivative anticancer candidate LaSOM 65 in rats. Xenobiotica.2014 Mar;44(3):254-63.
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氨基酸的分类：1、根据侧链基团的极性①非极性氨基酸（疏水氨基酸）8种丙氨酸（Ala）缬氨酸（Val）亮氨酸（Leu）异亮氨酸（Ile）脯氨酸（Pro）苯丙氨酸（Phe）色氨酸（Trp）蛋氨酸（Met）②极性氨基酸（亲水氨基酸）：极性不带电荷：7种甘氨酸（Gly）丝氨酸（Ser）苏氨酸（Thr）半胱氨酸（Cys）酪氨酸（Tyr）天冬酰胺（Asn）谷氨酰胺（Gln）极性带正电荷的氨基酸（碱性氨基酸） 3种 赖氨酸（Lys）精氨酸（Arg）组氨酸（His）极性带负电荷的氨基酸（酸性氨基酸） 2种 天冬氨酸（Asp）谷氨酸（Glu）2、根据化学结构脂肪族氨基酸：丙、缬、亮、异亮、蛋、天冬、谷、赖、精、甘、丝、苏、半胱、天冬酰胺、谷氨酰胺芳香族氨基酸：苯丙氨酸、酪氨酸杂环族氨基酸：组氨酸、色氨酸杂环亚氨基酸：脯氨酸3、从营养学的角度①必需氨基酸（essential amino acid）： 指人体（或其它脊椎动物）不能合成或合成速度远不适应机体的需要，必需由食物蛋白供给，这些氨基酸称为必需氨基酸。成人必需氨基酸的需要量约为蛋白质需要量的20%～37%。共有8种其作用分别是：赖氨酸：促进大脑发育，是肝及胆的组成成分，能促进脂肪代谢，调节松果腺、乳腺、黄体及卵巢，防止细胞退化；色氨酸：促进胃液及胰液的产生；苯丙氨酸：参与消除肾及膀胱功能的损耗；蛋氨酸（甲硫氨酸）：参与组成血红蛋白、组织与血清，有促进脾脏、胰脏及淋巴的功能；苏氨酸：有转变某些氨基酸达到平衡的功能；异亮氨酸：参与胸腺、脾脏及脑下腺的调节以及代谢；脑下腺属总司令部作用于甲状腺、性腺；亮氨酸：作用平衡异亮氨酸；缬氨酸：作用于黄体、乳腺及卵巢。②半必需氨基酸和条件必需氨基酸：精氨酸：精氨酸与脱氧胆酸制成的复合制剂（明诺芬）是主治梅毒、病毒性黄疸等病的有效药物。组氨酸：可作为生化试剂和药剂，还可用于治疗心脏病，贫血，风湿性关节炎等的药物。人体虽能够合成精氨酸和组氨酸，但通常不能满足正常的需要，因此，又被称为半必需氨基酸或条件必需氨基酸，在幼儿生长期这两种是必需氨基酸。人体对必需氨基酸的需要量随着年龄的增加而下降，成人比婴儿显著下降。（近年很多资料和教科书将组氨酸划入成人必需氨基酸）③非必需氨基酸（nonessentialamino acid）：指人（或其它脊椎动物）自己能由简单的前体合成，不需要从食物中获得的氨基酸。例如甘氨酸、丙氨酸等氨基酸。
第一次发帖，生怕叙述不清。
请问有哪位大神做过几个同源基因氨基酸序列保守性的图，本人做了一篇几个同源基因的SNP与疾病相关性的研究，投稿后，reviewer给的意见是，希望做一副这几个同源基因的氨基酸序列比对结果图，标注保守序列，我会查，但是不知道怎么做图，截屏么？还是有什么专用的软件？谢谢大家！
类似这样，但这个图是不同物种的同一基因序列保守性分析的图
20种蛋白质氨基酸都是α氨基酸。
其中除了甘氨酸外，其他氨基酸都具有旋光性，旋光性是由分子的空间构象引起的，你可以理解成像你的手掌一样，左右手的指头位置不同导致左右手的区别。根据旋光性分为L型（左型）和D型（右型）两种。
组成生命的氨基酸基本上都是L型。
